强效且口服有效的基于双噻唑的组蛋白去乙酰化酶抑制剂。
Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors.
作者信息
Chen Fei, Chai Hui, Su Ming-Bo, Zhang Yang-Ming, Li Jia, Xie Xin, Nan Fa-Jun
机构信息
Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , 189 Guoshoujing Road, Shanghai, 201203, China.
出版信息
ACS Med Chem Lett. 2014 Apr 4;5(6):628-33. doi: 10.1021/ml400470s. eCollection 2014 Jun 12.
Abstract
Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.
摘要
受天然产物拉戈唑中噻唑-噻唑啉帽基的启发，制备并评估了一系列结构简化的基于双噻唑的组蛋白去乙酰化酶抑制剂。化合物8f在实验性自身免疫性脑脊髓炎（EAE）模型中进行了体内评估，发现其口服给药对改善EAE小鼠的临床症状有效。
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